title: S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges.
abstract: BACKGROUND
  The recent introduction of integrase inhibitors (INIs) into the HIV treatment armentarium has had a significant impact on HIV treatment. However, at present, raltegravir twice daily is the only licensed INI featuring a lower genetic barrier compared with boosted protease inhibitors. S/GSK1349572 represents a new INI in current development. It is a once-daily, unboosted INI with low pharmacokinetic variability and predictable exposure-response relationship. Phase IIb studies in antiretroviral-naïve patients have demonstrated non-inferiority to efavirenz-based HIV therapy. Phase II studies in INI-experienced patients show partially retained activity in vivo. Overall, the safety profile of S/GSK1349572 in all studies completed has been very favorable.
  
  
  METHODS
  A Pubmed and Medline search was carried out on all articles on S/GSK1349572 from 2005 to 2010, including recent abstract presentations from major HIV conferences (CROI 2010, WAC2010, EACS2009, HIV10 and ICAAC2010). The reader will become acquainted with the unique properties of this new INI and will understand the current promises and challenges of the data available from S/GSK1349572.
  
  
  CONCLUSIONS
  S/GSK1349572 represents a new, unboosted, once-daily INI in development with distinct pharmacokinetics and resistance profile, which has showed promising potency and tolerability in the first clinical studies.
authors.affiliation: University of Bonn, Medicine I, Bonn, Germany.
authors.forename: Johannes Carl Christoph
authors.initials: JC
authors.lastname: Lenz
authors.forename: Jürgen Kurt
authors.initials: JK
authors.lastname: Rockstroh
mesh_terms: D000873:Anthracenes / Q000494:pharmacology* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D015507:Drugs, Investigational / Q000494:pharmacology* / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use*; D006575:Heterocyclic Compounds, 3-Ring; D006801:Humans; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D000099226:Dolutegravir
chemical_list: D000873:Anthracenes; D015507:Drugs, Investigational; D019428:HIV Integrase Inhibitors; D006575:Heterocyclic Compounds, 3-Ring; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D000099226:Dolutegravir